Tumor targeting agents and uses thereof
A technology of tumor targeting and detection agents, applied in the field of tumor targeting agents, can solve the problems of resistance reducing the effectiveness of available drugs, failure to reveal tumors, and undiscovered problems
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[0327] Preparation of targeting unit and targeting agent of the present invention
[0328] The targeting unit according to the invention is preferably a synthetic peptide. Peptides can be synthesized by various known techniques, such as solid phase synthesis methods (FMOC, BOC and other protection schemes, various resin types), solution phase synthesis methods (FMOC, BOC and other variants) and combinations thereof. Even automated synthesis apparatus / equipment are commercially available for this purpose, as are routine synthesis and purification services. These methods are well known to those skilled in the art. Some methods and materials are described, for example, in the following references:
[0329] Bachem AG, SASRIN TM (1999), The BACHEM Practice of SPPS (2000), Bachem 2001 catalog (2001), Novabiochem 2000 Catalog (2000), Peptide and Peptidomimetic Synthesis (2000) and The Combinatorial Chemistry Catalog & Solid Phase Organic Chemistry (SPOC) 9 Handbook 98 / 9. The synt...
Embodiment 1
[0380] Synthesis of targeting unit (peptide) LRS
[0381] A resin-bound targeting unit (protected peptide) containing the targeting motif LRS, protected with a functional group, was synthesized using the method described in Example 2.
[0382] The following reagents were used as starting materials (in the order given):
[0383] Fmoc-Ser(tBu) resin, Applied Biosystems catalog number 401429, 0.64 mmol / g
[0384] Fmoc-L-Arg(Pbf)-OH, CAS No. 154445-77-9, Applied Biosystems Catalog No. GEN911097, Molecular Weight: 648.8 g / mol
[0385] Fmoc-L-Leu-OH, CAS No. 35661-60-0, Applied Biosystems Catalog No. GEN911048, molecular weight: 353.4 g / mol
[0386] After the last cycle of the coupling procedure, a small sample of the resin-bound peptide was subjected to Fmoc removal (steps 1–10 in Example 2) and then treated with the excision mixture for 3 h as described in Example 2 Peptides are cleaved from the resin and separated. The product (LRS) was identified with the aid of its positive...
Embodiment 2
[0393] General description of the manual solid-phase peptide synthesis and mass spectrometric measurements used for the synthetic peptides described in the examples
[0394] All syntheses were carried out in a sealable glass funnel equipped with a sintered glass filter disc of porosity class 2 to 4 and topped with a polypropylene or phenolic plastic screw cap (for sealing), and two PTFE pushbutton pistons: one located under the filter disc (for draining) and the other at a beveled angle on the neck shoulder of the screw cap tube (for argon gas entry).
[0395] Fill the funnel with the appropriate solid-phase synthetic resin and solution for each treatment and place in a shaker flask shaker (Gallenkamp TM ) "wrist motion" for an appropriate period of time, followed by filtration under a moderate pressure of argon.
[0396] The general procedure of one synthesis cycle (=addition of one amino acid unit) is as follows:
[0397] will be loaded with about 1 mmol of Fmoc-peptide (=...
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